2. GPCR/G Protein
  3. Adenosine Receptor
  4. A2A receptor antagonist 1

A2A receptor antagonist 1  (Synonyms: CPI-444 analog)

Cat. No.: HY-102024 Purity: 99.96%
COA Handling Instructions

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A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively.

For research use only. We do not sell to patients.

A2A receptor antagonist 1 Chemical Structure

A2A receptor antagonist 1 Chemical Structure

CAS No. : 443103-97-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 82 In-stock
Solution
10 mM * 1 mL in DMSO USD 82 In-stock
Solid
1 mg USD 80 In-stock
5 mg USD 120 In-stock
10 mg USD 190 In-stock
50 mg USD 760 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

A2A receptor antagonist 1 Related Antibodies

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View All Adenosine Receptor Isoform Specific Products:

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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  • Purity & Documentation

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Description

A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively[1].
IC50 & Target

Ki: 4 nM (adenosine A2A receptor), 264 nM (A1 receptor)[1]
In Vitro

A2A receptor antagonist 1 (CPI-444 analog) is a potent adenosine A2A receptor antagonist, selective over the A1 receptor and demonstrates its binding activity with Ki values of 4 and 264 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A2A receptor antagonist 1 Related Antibodies
Molecular Weight

309.30

Formula

C16H12FN5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(C2=CC=CO2)=C3C(N(CC4=C(F)C=CC=C4)N=C3)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (80.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2331 mL 16.1655 mL 32.3311 mL
5 mM 0.6466 mL 3.2331 mL 6.4662 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.96%

COA (254 KB) HNMR (276 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2331 mL 16.1655 mL 32.3311 mL 80.8277 mL
5 mM 0.6466 mL 3.2331 mL 6.4662 mL 16.1655 mL
10 mM 0.3233 mL 1.6166 mL 3.2331 mL 8.0828 mL
15 mM 0.2155 mL 1.0777 mL 2.1554 mL 5.3885 mL
20 mM 0.1617 mL 0.8083 mL 1.6166 mL 4.0414 mL
25 mM 0.1293 mL 0.6466 mL 1.2932 mL 3.2331 mL
30 mM 0.1078 mL 0.5389 mL 1.0777 mL 2.6943 mL
40 mM 0.0808 mL 0.4041 mL 0.8083 mL 2.0207 mL
50 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6166 mL
60 mM 0.0539 mL 0.2694 mL 0.5389 mL 1.3471 mL
80 mM 0.0404 mL 0.2021 mL 0.4041 mL 1.0103 mL
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A2A receptor antagonist 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A2A receptor antagonist 1443103-97-7CPI-444CPI444CPI 444Adenosine ReceptorP1 receptorhypolocomotionmodelParkinsondiseaseInhibitorinhibitorinhibit

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